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Effects of 4-Nitrobenzofurazans and Their N-Oxides on Synthesis of Protein and Nucleic Acid by Murine Leukemia Cells¹

Departments of Oncology and Pharmacology, Wayne State University School of Medicine, and the Michigan Cancer Foundation, Detroit, Michigan 48201 [D. K.], and the Laboratories, Medical Research Council of Ireland, Trinity College, Dublin [J. G. B.]

A series of benzo-2,1,3-oxadiazoles (benzofurazans) and their N-oxides (benzofuroxans) inhibit incorporation of precursors into nucleic acids and protein by murine leukemia cells. At slightly higher levels, substantial single- and double-strand DNA breakage was observed. At still higher concentrations, inhibition of phosphorylation of uridine and thymidine was found. Structure-activity relationships show that only compounds bearing appropriate substitutions at positions 4 and 7 were effective inhibitors of biosynthetic pathways. Such compounds appear to interact with a wide variety of biological systems and may be useful in elucidating modes of macromolecule synthesis.

¹ Supported in part by Grants CA-16053 and CA-07177 from the National Cancer Institute, NIH, and by the Irish Cancer Society.

² To whom requests for reprints should be addressed, at Darling Memorial Center, 4160 John R Street, Detroit, Mich. 48201.

Received 3/20/75. Accepted 9/ 9/75.

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